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Open AccessArticle

Acetal-Linked Paclitaxel Polymeric Prodrug Based on Functionalized mPEG-PCL Diblock Polymer for pH-Triggered Drug Delivery

by Yinglei Zhai 1,2,†, Xing Zhou 3,†, Lina Jia 4, Chao Ma 5, Ronghua Song 1, Yanhao Deng 1, Xueyao Hu 1 and Wei Sun 1,*
1
Department of Biomedical Engineering, School of Medical Devices, Shenyang Pharmaceutical University, Shenyang 110016, China
2
State Key Laboratory for Marine Corrosion and Protection, Luoyang Ship Material Research Institute (LSMRI), Qingdao 266101, China
3
Hainan Institute of Materia Medica, Haikou 570311, China
4
Department of Pharmacology, School of Life Science and Biopharmaceutics, Shenyang Pharmaceutical University, Shenyang 110016, China
5
College of Food & Pharmaceutical Engineering, Guizhou Institute of Technology, Guizhou 550003, China
*
Author to whom correspondence should be addressed.
These two authors contributed equally to this work
Polymers 2017, 9(12), 698; https://doi.org/10.3390/polym9120698
Received: 14 October 2017 / Revised: 17 November 2017 / Accepted: 7 December 2017 / Published: 11 December 2017
(This article belongs to the Special Issue Polymer Micelles)
The differences in micro-environment between cancer cells and the normal ones offer the possibility to develop stimuli-responsive drug-delivery systems for overcoming the drawbacks in the clinical use of anticancer drugs, such as paclitaxel, doxorubicin, and etc. Hence, we developed a novel endosomal pH-sensitive paclitaxel (PTX) prodrug micelles based on functionalized poly(ethylene glycol)-poly(ε-caprolactone) (mPEG-PCL) diblock polymer with an acid-cleavable acetal (Ace) linkage (mPEG-PCL-Ace-PTX). The mPEG-PCL-Ace-PTX5 with a high drug content of 23.5 wt % was self-assembled in phosphate buffer (pH 7.4, 10 mM) into nanosized micelles with an average diameter of 68.5 nm. The in vitro release studies demonstrated that mPEG-PCL-Ace-PTX5 micelles was highly pH-sensitive, in which 16.8%, 32.8%, and 48.2% of parent free PTX was released from mPEG-PCL-Ace-PTX5 micelles in 48 h at pH 7.4, 6.0, and 5.0, respectively. Thiazolyl Blue Tetrazolium Bromide (MTT) assays suggested that the pH-sensitive PTX prodrug micelles displayed higher therapeutic efficacy against MCF-7 cells compared with free PTX. Therefore, the PTX prodrug micelles with acetal bond may offer a promising strategy for cancer therapy. View Full-Text
Keywords: prodrug; polymer micelles; pH-sensitive; acetal; paclitaxel prodrug; polymer micelles; pH-sensitive; acetal; paclitaxel
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MDPI and ACS Style

Zhai, Y.; Zhou, X.; Jia, L.; Ma, C.; Song, R.; Deng, Y.; Hu, X.; Sun, W. Acetal-Linked Paclitaxel Polymeric Prodrug Based on Functionalized mPEG-PCL Diblock Polymer for pH-Triggered Drug Delivery. Polymers 2017, 9, 698.

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